| Antiplasmodials from natural resources 2010-2019 | ||||
| Degotte G, Pirotte B, Francotte P, Frédérich M. Overview of natural antiplasmodials from the last decade to inspire medicinal chemistry. Curr Med Chem. 2021 Mar 29. PMID: 33781183. pub ahead of print. | ||||
| Compound | Antiplasmodial Strains | IC50 (µM) | ||
| Antiplasmodial & cytotoxic activities of reported flavonoid structures | ||||
| Luteolin 7-O-glucoside | TM4/8.2 | 6.2 ± 2.2 | ||
| K1CB1 | 4.5 ± 2.2 | |||
| Quercetin 3-O-beta D-glucopyranoside | 3D7 | 5.5 | ||
| Dd2 | 4.1 | |||
| D6 | 43 ± 0.3 | |||
| W2 | 106 ± 1 | |||
| Volkensifkvone | F32 | 1.8 ± 1.2 | ||
| FcM29 | 1.7 ± 3.7 | |||
| Chamaejasmin | Pf | 4.3 | ||
| (3E,3'E)-1,1'-(((2S,3R,4R,5S,6S)-2-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-5-hydroxy-6-methyltetrahydro-2H-pyran-3,4-diyl)bis(oxy))bis(4-(4-hydroxyphenyl)but-3-en-2-one) | HB3 | 0.6 ± 0.2 | NA | |
| NHP1337 | 7 ± 1 | NA | ||
| (3E,3'E)-1,1'-(((2S,3R,4R,5S,6S)-2-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-5-hydroxy-6-methyltetrahydro-2H-pyran-3,4-diyl)bis(oxy))bis(4-(4-hydroxyphenyl)but-3-en-2-one) | HB3 | 2 ± 0.6 | NA | |
| NHP1337 | 4 ± 1.0 3 | NA | ||
| 5,7-dihydroxy-3-(((2S,3R,4R,5S,6S)-5-hydroxy-4-(((E)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)-3-(((Z)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)-6-methyltetrahydro-2H-pyran-2-yl)oxy)-2-(4-hydroxyphenyl)-4H-chromen-4-one | HB3 | 0.5 ± 0.03 | NA | |
| NHP1337 | 4.1 ± 0.5 | NA | ||
| (3Z,3'Z)-1,1'-(((2S,3R,4R,5S,6S)-2-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-5-hydroxy-6-methyltetrahydro-2H-pyran-3,4-diyl)bis(oxy))bis(4-(4-hydroxyphenyl)but-3-en-2-one) | HB3 | 1.8 ± 0.4 | NA | |
| NHP1337 | 7 ± 1 2 | NA | ||
| (2R,3R,4S,5R,6S)-6-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-4-(((E)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)-2-((E)-5-(4-hydroxyphenyl)-3-oxopent-4-en-1-yl)-5-methoxytetrahydro-2H-pyran-3-yl acetate | HB3 | 0.6 ± 0.1 | NA | |
| NHP1337 | 2.1 ± 0.6 | NA | ||
| (2R,3R,4S,5R,6S)-6-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-4-(((E)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)-2-((Z)-5-(4-hydroxyphenyl)-3-oxopent-4-en-1-yl)-5-methoxytetrahydro-2H-pyran-3-yl acetate | HB3 | 0.9 ± 0.2 | NA | |
| NHP1337 | 5 ± 1 | NA | ||
| (2R,3R,4S,5R,6S)-6-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-4-(((Z)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)-2-((((E)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)methyl)-5-methoxytetrahydro-2H-pyran-3-yl acetate | HB3 | 0.8 ± 0.1 | NA | |
| (2R,3R,4S,5R,6S)-6-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-4-(((E)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)-2-((((Z)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)methyl)-5-methoxytetrahydro-2H-pyran-3-yl acetate | NHP1337 | 4 ± 1 | NA | |
| (2R,3R,4S,5R,6S)-6-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-3-yl)oxy)-4-(((E)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)-2-((((E)-4-(4-hydroxyphenyl)-2-oxobut-3-en-1-yl)oxy)methyl)-5-methoxytetrahydro-2H-pyran-3-yl acetate | HB3 | 2.1 ± 0.9 | NA | |
| NHP1337 | 3.8 ± 0.6 | NA | ||
| Lonchocarpol | Pf | 4.1 | ||
| MS-II | D6 | 4.6 ± 1.1 | ||
| 3D7 | 1.7 ± 0.1 | |||
| KSM009 | 1.5 ± 0.1 | |||
| Carphorin B | Dd2 | 3.4 ± 0.4 | ||
| Torellianone E | 3D7 | 3.2 ± 0.3 | NA | |
| Dauphinol A | Dd2 | 4.7 ± 0.3 | NA | |
| Dauphinol B | Dd2 | 0.8 ± 0.1 | NA | |
| (2S)-7-O-galloyl-5,3',4-trihydroxyflavan | K1 | 0.6 | ||
| Antiplasmodial activities of reported phenolic compounds | ||||
| (2S)-7,3-O-digalloyl-5,4'-dihydroxyflavan | K1 | 1.4 | ||
| Sigmoidin A | K1 | 3 | ||
| Sigmoidin F | K1 | 2.3 | ||
| 4'-O-methylsigmoidin B | K1 | 2.3 | ||
| K1 | 4.4 | |||
| K1 | 4.4 | |||
| Abyssinin III | K1 | 2.3 | ||
| Lophirone E | 3D7 (asex.) | 38.5 ± 3.2 | ||
| W2 (asex.) | 12.2 ± 2.1 | |||
| 3D7 (gam.) | 0.1 ± 0.04 | |||
| Alpha'-chlorophirone | 3D7 (asex.) | >50 | NA | |
| W2 (asex.) | 17.9 ± 5 42 | |||
| 3D7 (gam.) | 4.1 ± 1.4 43 |
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| Lakoochanoside B | K1 | 2.8 | NA | |
| Cycloartocarpin | K1 | 2.7 | ||
| 5'-prenyl-pratensein | K1 | 2.9 | NA | |
| 4-{2-rel-(1R,3R,5S)-7-oxo-2,6-dioxabicyclo[3.3.1]non-3-yl]ethyl}phenyl 3,4,5-trihydroxybenzoate | NF54 | 2.4 ± 0.5 | NA | |
| Methyl gallate | 3D7 | 4.9 ± 3.3 | ||
| 3D7 | 1.1 ± 0.2 | |||
| Dd2 | 1.6 ± 0.2 | |||
| Ethyl gallate | Dd2 | 9.3 ± 3.1 | ||
| D6 | 7 | |||
| W2 | 4.2 | |||
| Lauryl gallate | Dd2 | 2.2 ±0 .2 | ||
| 2-(6-benzoyl-beta--D-glucopyranosyloxy)-7-(1-alpha, 2-alpha, 6-alpha-trihydroxy-3-oxocyclohex-4-enoyl-5-hydroxybenzyl alcohol | 3D7 | 3.2 ± 0.1 | NA | |
| Ellagic acid | W2 | 0.7 ± 0.02 | NA | |
| Achyroclinopyrone A | NF54 | 3.8 ± 0.6 | NA | |
| Achyroclinopyrone B | NF54 | 1.2 ± 0.01 | NA | |
| 16Z/E-Achyroclinopyrone D | NF54 | 2.6 ± 0.1 | NA | |
| 23-methyl-6-O-desmethylaurecepyrone | NF54 | 2.5 ± 0.1 | NA | |
| Cladophorol A | Dd2 | 2.7 | ||
| Cladophorol B | Dd2 | 4.1 | ||
| Acronylin | 3D7 | 1.8 | ||
| Spyroaxillarone A | Dd2 | 3.1 | NA | |
| K1 | 2.3 | NA | ||
| Uvarin B | K1 | 4.8 ± 0.4 | NA | |
| Uvarin C | K1 | 4.9 ± 0.3 | NA | |
| 4-O-geranylisoliquiritigenin | 3D7 | 3.7 | ||
| Dd2 | 7 | |||
| Moracin C | K1 | 3.5 | ||
| Arcotrione | 3D7 | 2.4 | NA | |
| Dd2 | 4.7 | NA | ||
| Xanthoquinodine A6 | K1 | 0.9 | NA | |
| Ketoxnthoquinodine A6 | K1 | 3.7 | NA | |
| Xanthoquinodine B4 | K1 | 0.5 | NA | |
| Xanthoquinodine B5 | K1 | 0.9 | NA | |
| MDN-0185 | 3D7 | 0.009 | ||
| Secalonic acid F | K1 | 2.2 | ||
| Macluraxanthone | F32 | 1.2 ± 0.3 | ||
| FcM29 | 0.9 ± 0.2 | |||
| Luteoskyrin | K1 | 0.9 | ||
| Knipholone X | 3D7 | 1.93 | ||
| HB3 | 4.9 ± 0.6 | |||
| NHP1337 | 5 ± 2 | |||
| Knipholone anthrone X | 3D7 | 0.7 | ||
| Mansonone D | K1 | 2.3 | ||
| 4'-methylhonokiol | Dd2 | 2.8 ± 0.1 | ||
| Magnolol | Dd2 | 3.4 ± 0.1 | ||
| Ent-mururin A | K1 | 4.7 ± 2.9 | NA | |
| Antiplasmodial activities of reported terpenoid molecules | ||||
| Iso-mukaadial acetate | D6 | 4.9 ± 1.9 | ||
| W2 | 3.6 ± 0.3 | |||
| Trichodermin | NF54 | 1.4 ± 0.3 | ||
| 6'12'-epoxymyrotoxin A | K1 | 0.1 | NA | |
| K1 | 0.002 | NA | ||
| 7'-hydroymitoxin B | K1 | 0.002 | NA | |
| Miotoxin A | K1 | 0.002 | ||
| Smenotronic acid | K1 | 0.002 | ||
| Ilimaquinone | D6 | 3.9 ± 0.3 | ||
| W2 | 2.3 ± 0.3 | |||
| Pelorol | Dd2 | 3.5 ± 0.6 | ||
| Neoboutomacroin | Dd2 | 2.1 ± 0.2 | ||
| Montanin | Dd2 | 0.8 ± 0.2 | ||
| Cyathinin A | K1 | 2.1 | ||
| Stratin C | K1 | 1.4 | ||
| Striatal A | K1 | 1 | ||
| Striatal B | K1 | 0.9 | ||
| Striatal C | K1 | 2.1 | ||
| Ferruginol | NF54 | 2.9 | ||
| Leriifoliol | NF54 | 0.4 ± 0.1 | ||
| Leriifolione | NF54 | 3.6 ± 0.2 | ||
| Antiplasmodial activities of reported triterpenoid structures | ||||
| Peyssonnoside A | Dd2 | >6.3 | ||
| D10 | >6.3 | |||
| 3-O-acetyloleuritolic acid | D6 | 15 ± 1.6 | ||
| W2 | 4.5 ± 1.1 | |||
| (1R,3aS,5aR,5bR,8S,9S,11aR)-3a-(hydroxymethyl)-8-((Z)-5-(4-hydroxyphenyl)-3-methylenepent-4-en-1-yl)-5a,5b,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-ol | HB3 | 0.9 ± 0.1 | NA | |
| NHP1337 | 0.9 ± 0.1 | NA | ||
| (1R,3aS,5aR,5bR,8S,9S,11aR)-3a-(hydroxymethyl)-8-((Z)-5-(3-hydroxyphenyl)-3-methylenepent-4-en-1-yl)-5a,5b,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-ol | HB3 | 0.8 ± 0.4 | NA | |
| NHP1337 | 1.5 ± 0.1 | NA | ||
| ((1R,3aS,5aR,5bR,8R,9S,11aR)-9-hydroxy-5a,5b,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-3aH-cyclopenta[a]chrysene-3a,8-diyl)dimethanol | HB3 | 3.4 ± 0.5 | NA | |
| NHP1337 | 5.2 ± 0.3 | NA | ||
| (1R,3aS,5aR,5bR,8R,9S,11aR)-3a,8-bis(hydroxymethyl)-5a,5b,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl (E)-3-(4-hydroxyphenyl)acrylate | HB3 | 1.9 ± 0.2 | NA | |
| NHP1337 | 1.4 ± 0.2 | NA | ||
| (E)-4-(4-hydroxy-3-methoxyphenyl)-1-(((1R,3aS,5aR,5bR,8R,9S,11aR)-3a-(hydroxymethyl)-9-methoxy-5a,5b,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-8-yl)methoxy)but-3-en-2-one | HB3 | 0.5 ± 0.2 | NA | |
| NHP1337 | 0.3 ± 0.03 | |||
| Polycarpol | K1 | 3.0± 3.3 | ||
| 3-O-beta-D-glucopyranoside-sitosterol | 3D7 | 3.2± 0.4 | NA | |
| Dd2 | 9.0± 1.7 | NA | ||
| 3D7 | 32± 3.3 | NA | ||
| INDO | >34 | NA | ||
| Isoflindissol lactone | NF54 | 2.2 | ||
| Eurycomanone | NF54 | 4.2 | ||
| Eurycomanol | 3D7 | 0.005 | ||
| Isoflindissone lactone | 3D7 | 0.4 | ||
| 18-dehydro-6- alpha-hydroxyeury comalactone | 3D7 | 0.3 | NA | |
| Perovkone C | NF54 | 0.6 | NA | |
| Perovkone E | NF54 | 1.3 | NA | |
| Perovkone F | NF54 | 3.6 | NA | |
| Salvadione D | NF54 | 1.9 | ||
| Salvadione A | NF54 | 1.1 | ||
| Variecolin | K1 | 4 | ||
| 3-O-acetyl-7-O-benzoyl ceanotic acid methylester | K1 | 4.6 | NA | |
| Halymeniaol | 3D7 | 3 | ||
| Ganoderic acid AW1 | D6 | 0.3 | ||
| W2 | 2 | |||
| Kaimanol | 3D7 | 0.4 | ||
| Saringosterol | 3D7 | 0.00025 | ||
| Grandifolione | K1 | 1.4 | ||
| 7-deacetylkhivorine | K1 | 2.5 | ||
| Kotschienone A | 3D7 | 2.4± 0.2 | ||
| Kotschienone B | INDO | 2.6±0.4 | ||
| 3D7 | 1.7± 0.3 | NA | ||
| INDO | 1.7± 0.3 | NA | ||
| 7-deacetylgedunin | 3D7 | 4.2± 0.7 | ||
| INDO | 5.1± 0.5 | |||
| 7-deacetyl-7-deoxogedunin | 3D7 | 6.1± 1.1 | NA | |
| INDO | 4.5± 1.5 | NA | ||